BRPI0616374B8 - form i of the phosphate salt of a 2-indolinone substituted pyrrole compound, pharmaceutical composition, uses and method of preparation of form i - Google Patents
form i of the phosphate salt of a 2-indolinone substituted pyrrole compound, pharmaceutical composition, uses and method of preparation of form iInfo
- Publication number
- BRPI0616374B8 BRPI0616374B8 BRPI0616374A BRPI0616374A BRPI0616374B8 BR PI0616374 B8 BRPI0616374 B8 BR PI0616374B8 BR PI0616374 A BRPI0616374 A BR PI0616374A BR PI0616374 A BRPI0616374 A BR PI0616374A BR PI0616374 B8 BRPI0616374 B8 BR PI0616374B8
- Authority
- BR
- Brazil
- Prior art keywords
- pharmaceutical composition
- indolinone
- phosphate salt
- polymorphs
- preparation
- Prior art date
Links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Endocrinology (AREA)
- Transplantation (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
formas de sal sólido para um pirrol substituído 2-indolinona, composição farmacêutica compreendendo as mesmas, método para modulação de atividade catalítica de proteína quinase, proteína quinase, métodos para preparação de cristais e de polimorfos e uso. a presente invenção refere-se a formas de sal sólido de um composto 3-pirrol substituído 2-indolinona, (2-pirrolidina-1-ii-etil)-amida de ácido 5-[5-flúor-2-oxo-1 ,2-di-hidro-indol-(3z)-ilidenometil]-2 ,4-dimetil-1h-pirrol-3- carboxílico. também refere-se a polimorfos do sal fosfato da amida. a invenção ainda refere-se ao uso dos sais e polimorfos no tratamento de distúrbios relacionados com proteína quinase.solid salt forms for a 2-indolinone substituted pyrrole, pharmaceutical composition comprising the same, method for modulating protein kinase catalytic activity, protein kinase, methods for preparing crystals and polymorphs and use. The present invention relates to solid salt forms of a 3-pyrrole substituted 2-indolinone compound, 5-[5-fluoro-2-oxo-1, acid (2-pyrrolidine-1-h-ethyl)-amide, 2-dihydro-indole-(3z)-ylidenemethyl]-2,4-dimethyl-1h-pyrrole-3-carboxylic acid. also refers to polymorphs of the phosphate salt of the amide. the invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71858605P | 2005-09-19 | 2005-09-19 | |
| US60/718,586 | 2005-09-19 | ||
| PCT/IB2006/002506 WO2007034272A1 (en) | 2005-09-19 | 2006-09-08 | Solid salt forms of a pyrrole substituted 2-indolinone |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0616374A2 BRPI0616374A2 (en) | 2011-06-21 |
| BRPI0616374B1 BRPI0616374B1 (en) | 2020-05-12 |
| BRPI0616374B8 true BRPI0616374B8 (en) | 2021-05-25 |
Family
ID=37626412
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0616374A BRPI0616374B8 (en) | 2005-09-19 | 2006-09-08 | form i of the phosphate salt of a 2-indolinone substituted pyrrole compound, pharmaceutical composition, uses and method of preparation of form i |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US20080275101A1 (en) |
| EP (2) | EP1928858B1 (en) |
| JP (2) | JP4519114B2 (en) |
| KR (1) | KR101050906B1 (en) |
| CN (2) | CN103601720B (en) |
| AR (1) | AR056521A1 (en) |
| AU (1) | AU2006293644B2 (en) |
| BR (1) | BRPI0616374B8 (en) |
| CA (1) | CA2621569C (en) |
| CY (1) | CY1109326T1 (en) |
| DE (1) | DE602006008015D1 (en) |
| DK (1) | DK1928858T3 (en) |
| ES (1) | ES2328407T3 (en) |
| IL (1) | IL189590A0 (en) |
| MX (1) | MX2008002415A (en) |
| NO (1) | NO20080866L (en) |
| NZ (1) | NZ566033A (en) |
| PL (1) | PL1928858T3 (en) |
| PT (1) | PT1928858E (en) |
| RU (1) | RU2399619C2 (en) |
| SI (1) | SI1928858T1 (en) |
| TW (1) | TWI310766B (en) |
| WO (1) | WO2007034272A1 (en) |
| ZA (1) | ZA200801431B (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1928858T3 (en) | 2005-09-19 | 2009-10-26 | Pfizer Prod Inc | Solid salt forms of a pyrrole-substituted 2-indolinone |
| US20100189788A1 (en) | 2009-01-23 | 2010-07-29 | Teva Pharmaceutical Industries, Ltd. | Delayed release rasagiline base formulation |
| CN102858739A (en) | 2010-03-10 | 2013-01-02 | 斯索恩有限公司 | A process for amidation of pyrrole carboxylate compounds |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2155187C2 (en) * | 1992-08-06 | 2000-08-27 | Варнер-Ламберт Компани | Derivatives of indole, their tautomers, mixtures of their isomers or separate isomers and pharmaceutically acceptable salts, pharmaceutical composition showing antitumor or inhibiting protein tyrosine kinase activity and method of inhibition of protein tyrosine kinase-depending disease or control of aberrant growth of mammalian or human cells |
| US6574293B1 (en) | 1998-10-28 | 2003-06-03 | Ericsson Inc. | Receivers and methods for reducing interference in radio communications |
| PT1255536E (en) * | 1999-12-22 | 2006-09-29 | Sugen Inc | DERIVATIVES OF INDOLINONE FOR THE MODULATION OF TYROSINE PROTEIN CINASE TYPE C-KIT |
| PT1255752E (en) * | 2000-02-15 | 2007-10-17 | Pharmacia & Upjohn Co Llc | Pyrrole substituted 2-indolinone protein kinase inhibitors |
| WO2002081466A1 (en) * | 2001-04-09 | 2002-10-17 | Sugen, Inc. | Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives |
| DK3168218T3 (en) | 2001-08-15 | 2019-01-14 | Pharmacia & Upjohn Co Llc | Crystalline comprising an L-malic acid salt of N- [2- (DIETHYLAMINO) ETHYL] -5 - [(5-FLUOR-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDE) METHYL] -2,4 -DIMETHYL-1H-PYRROL-3-CARBOXAMIDE FOR USE AS A MEDICINE |
| MXPA04006992A (en) * | 2002-02-15 | 2004-11-10 | Upjohn Co | Process for preparing indolinone derivatives. |
| US7452913B2 (en) * | 2003-02-24 | 2008-11-18 | Pharmacia & Upjohn Company | Polymorphs of pyrrole substituted 2-indolinone protein kinase inhibitors |
| US20040209937A1 (en) * | 2003-02-24 | 2004-10-21 | Sugen, Inc. | Treatment of excessive osteolysis with indolinone compounds |
| US20060009510A1 (en) * | 2004-07-09 | 2006-01-12 | Pharmacia & Upjohn Company Llc | Method of synthesizing indolinone compounds |
| DK1928858T3 (en) | 2005-09-19 | 2009-10-26 | Pfizer Prod Inc | Solid salt forms of a pyrrole-substituted 2-indolinone |
-
2006
- 2006-09-08 DK DK06795470T patent/DK1928858T3/en active
- 2006-09-08 MX MX2008002415A patent/MX2008002415A/en active IP Right Grant
- 2006-09-08 RU RU2008109959/04A patent/RU2399619C2/en not_active IP Right Cessation
- 2006-09-08 KR KR1020087006545A patent/KR101050906B1/en active Active
- 2006-09-08 BR BRPI0616374A patent/BRPI0616374B8/en active IP Right Grant
- 2006-09-08 CA CA2621569A patent/CA2621569C/en active Active
- 2006-09-08 US US12/067,242 patent/US20080275101A1/en not_active Abandoned
- 2006-09-08 SI SI200630386T patent/SI1928858T1/en unknown
- 2006-09-08 CN CN201310478975.0A patent/CN103601720B/en active Active
- 2006-09-08 PT PT06795470T patent/PT1928858E/en unknown
- 2006-09-08 AU AU2006293644A patent/AU2006293644B2/en active Active
- 2006-09-08 PL PL06795470T patent/PL1928858T3/en unknown
- 2006-09-08 EP EP06795470A patent/EP1928858B1/en active Active
- 2006-09-08 EP EP09165944A patent/EP2112148A1/en not_active Withdrawn
- 2006-09-08 CN CN2006800345053A patent/CN101287724B/en active Active
- 2006-09-08 ES ES06795470T patent/ES2328407T3/en active Active
- 2006-09-08 DE DE602006008015T patent/DE602006008015D1/en active Active
- 2006-09-08 WO PCT/IB2006/002506 patent/WO2007034272A1/en not_active Ceased
- 2006-09-08 NZ NZ566033A patent/NZ566033A/en unknown
- 2006-09-15 JP JP2006250347A patent/JP4519114B2/en active Active
- 2006-09-18 TW TW095134445A patent/TWI310766B/en not_active IP Right Cessation
- 2006-09-19 AR ARP060104101A patent/AR056521A1/en not_active Application Discontinuation
-
2008
- 2008-02-18 IL IL189590A patent/IL189590A0/en unknown
- 2008-02-18 NO NO20080866A patent/NO20080866L/en not_active Application Discontinuation
- 2008-09-12 ZA ZA200801431A patent/ZA200801431B/en unknown
-
2009
- 2009-08-20 CY CY20091100887T patent/CY1109326T1/en unknown
- 2009-12-10 JP JP2009279987A patent/JP2010090152A/en active Pending
-
2012
- 2012-02-06 US US13/367,009 patent/US8987320B2/en active Active
-
2015
- 2015-02-12 US US14/620,835 patent/US9290479B2/en active Active
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